Assay Detail
Functional
CHEMBL899758
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Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.03 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL236521 | — | — | 1 | 7.72 |
| CHEMBL393576 | — | — | 1 | 7.68 |
| CHEMBL397582 | — | — | 1 | 7.46 |
| CHEMBL393788 | — | — | 1 | 7.36 |
| CHEMBL393204 | — | — | 1 | 7.32 |
| CHEMBL397583 | — | — | 1 | 7.28 |
| CHEMBL235640 | — | — | 1 | 7.28 |
| CHEMBL397584 | — | — | 1 | 7.10 |
| CHEMBL391028 | — | — | 1 | 7.03 |
| CHEMBL237365 | — | — | 1 | 7.00 |
| CHEMBL391914 | — | — | 1 | 6.66 |
| CHEMBL262320 | — | — | 1 | 6.47 |
| CHEMBL236940 | — | — | 1 | 6.44 |
| CHEMBL396433 | — | — | 1 | 6.34 |
| CHEMBL397580 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL236521 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL393576 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL397582 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL393788 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL393204 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL397583 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL235640 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL397584 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL391028 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL237365 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL391914 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL262320 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL236940 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL396433 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL397580 | — | IC50 | = | 480.0 | nM | 6.32 |